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<title>177Lu-DOTA-Tyr3-c(Cys-Tyr-Trp-Lys-Thr-Cys)-Thr-Lys(cypate)-NH2 - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf</title>
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<meta name="robots" content="INDEX,FOLLOW,NOARCHIVE" /><meta name="citation_inbook_title" content="Molecular Imaging and Contrast Agent Database (MICAD) [Internet]" /><meta name="citation_title" content="177Lu-DOTA-Tyr3-c(Cys-Tyr-Trp-Lys-Thr-Cys)-Thr-Lys(cypate)-NH2" /><meta name="citation_publisher" content="National Center for Biotechnology Information (US)" /><meta name="citation_date" content="2008/04/22" /><meta name="citation_author" content="Huiming Zhang" /><meta name="citation_pmid" content="20641372" /><meta name="citation_fulltext_html_url" content="https://www.ncbi.nlm.nih.gov/books/NBK23169/" /><link rel="schema.DC" href="http://purl.org/DC/elements/1.0/" /><meta name="DC.Title" content="177Lu-DOTA-Tyr3-c(Cys-Tyr-Trp-Lys-Thr-Cys)-Thr-Lys(cypate)-NH2" /><meta name="DC.Type" content="Text" /><meta name="DC.Publisher" content="National Center for Biotechnology Information (US)" /><meta name="DC.Contributor" content="Huiming Zhang" /><meta name="DC.Date" content="2008/04/22" /><meta name="DC.Identifier" content="https://www.ncbi.nlm.nih.gov/books/NBK23169/" /><meta name="description" content="Somatostatin (SST) (somatotropin release-inhibiting hormone, somatotropin release-inhibiting factor) is a cyclic disulphide-containing peptide hormone of 14 amino acids (1). SST inhibits hormone secretion, cell proliferation, and promotes apoptosis through binding to specific cell-surface somatostatin receptors (SSTRs) (2). Five SSTR subtypes are identified in the central nervous system (CNS), gastrointestinal tract, and a variety of benign and malignant tumors (2). All subtypes of SSTRs belong to the family of G protein–coupled receptors, and exhibit high affinity to SST by recognizing the β-turn in the peptide sequence of SST including Phe7, Trp8, Lys9, and Thr10 (2). The structural difference between SSTRs generates specific pharmacological and physiological properties for each subtype, which allows targeting of SSTRs with subtype-specific SST analogs (1). For example, octreotide, a SST analog with a peptide sequence of eight amino acids (D-Phe-c(Cys-Tyr-D-Trp-Lys-Thr-Cys)-Thr(ol)), possesses a much higher affinity (~2 nM) binding to SSTR-2, -3, and -5 than binding to SSTR-1 and -4 (>1,000 nM). In addition to symptomatic treatment of tumors in clinic, these analogs are also labeled with a variety of probes for imaging (1)." /><meta name="og:title" content="177Lu-DOTA-Tyr3-c(Cys-Tyr-Trp-Lys-Thr-Cys)-Thr-Lys(cypate)-NH2" /><meta name="og:type" content="book" /><meta name="og:description" content="Somatostatin (SST) (somatotropin release-inhibiting hormone, somatotropin release-inhibiting factor) is a cyclic disulphide-containing peptide hormone of 14 amino acids (1). SST inhibits hormone secretion, cell proliferation, and promotes apoptosis through binding to specific cell-surface somatostatin receptors (SSTRs) (2). Five SSTR subtypes are identified in the central nervous system (CNS), gastrointestinal tract, and a variety of benign and malignant tumors (2). All subtypes of SSTRs belong to the family of G protein–coupled receptors, and exhibit high affinity to SST by recognizing the β-turn in the peptide sequence of SST including Phe7, Trp8, Lys9, and Thr10 (2). The structural difference between SSTRs generates specific pharmacological and physiological properties for each subtype, which allows targeting of SSTRs with subtype-specific SST analogs (1). For example, octreotide, a SST analog with a peptide sequence of eight amino acids (D-Phe-c(Cys-Tyr-D-Trp-Lys-Thr-Cys)-Thr(ol)), possesses a much higher affinity (~2 nM) binding to SSTR-2, -3, and -5 than binding to SSTR-1 and -4 (>1,000 nM). 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<div class="pre-content"><div><div class="bk_prnt"><p class="small">NCBI Bookshelf. A service of the National Library of Medicine, National Institutes of Health.</p><p>Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013. </p></div><div class="iconblock clearfix whole_rhythm no_top_margin bk_noprnt"><a class="img_link icnblk_img" title="Table of Contents Page" href="/books/n/micad/"><img class="source-thumb" src="/corehtml/pmc/pmcgifs/bookshelf/thumbs/th-micad-lrg.png" alt="Cover of Molecular Imaging and Contrast Agent Database (MICAD)" height="100px" width="80px" /></a><div class="icnblk_cntnt eight_col"><h2>Molecular Imaging and Contrast Agent Database (MICAD) [Internet].</h2><a data-jig="ncbitoggler" href="#__NBK23169_dtls__">Show details</a><div style="display:none" class="ui-widget" id="__NBK23169_dtls__"><div>Bethesda (MD): <a href="https://www.ncbi.nlm.nih.gov/" ref="pagearea=page-banner&targetsite=external&targetcat=link&targettype=publisher">National Center for Biotechnology Information (US)</a>; 2004-2013.</div></div><div class="half_rhythm"><ul class="inline_list"><li style="margin-right:1em"><a class="bk_cntns" href="/books/n/micad/">Contents</a></li></ul></div><div class="bk_noprnt"><form method="get" action="/books/n/micad/" id="bk_srch"><div class="bk_search"><label for="bk_term" class="offscreen_noflow">Search term</label><input type="text" title="Search this book" id="bk_term" name="term" value="" data-jig="ncbiclearbutton" /> <input type="submit" class="jig-ncbibutton" value="Search this book" submit="false" style="padding: 0.1em 0.4em;" /></div></form></div></div><div class="icnblk_cntnt two_col"><div class="pagination bk_noprnt"><a class="active page_link prev" href="/books/n/micad/sos177lucypate/" title="Previous page in this title">< Prev</a><a class="active page_link next" href="/books/n/micad/sos64cucy5.5/" title="Next page in this title">Next ></a></div></div></div></div></div>
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<div class="main-content lit-style" itemscope="itemscope" itemtype="http://schema.org/CreativeWork"><div class="meta-content fm-sec"><h1 id="_NBK23169_"><span class="title" itemprop="name"><sup>177</sup>Lu-DOTA-Tyr<sup>3</sup>-c(Cys-Tyr-Trp-Lys-Thr-Cys)-Thr-Lys(cypate)-NH<sub>2</sub></span></h1><div itemprop="alternativeHeadline" class="subtitle whole_rhythm"><sup>177</sup>Lu-LS172</div><p class="contrib-group"><span itemprop="author">Huiming Zhang</span>, PhD.</p><a data-jig="ncbitoggler" href="#__NBK23169_ai__" style="border:0;text-decoration:none">Author Information and Affiliations</a><div style="display:none" class="ui-widget" id="__NBK23169_ai__"><div class="contrib half_rhythm"><span itemprop="author">Huiming Zhang</span>, PhD<div class="affiliation small">
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National Center for Biotechnology Information, NLM, NIH, Bethesda, MD,
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<span class="before-email-separator"></span><span class="email-label">Email: </span><a href="mailto:dev@null" data-email="vog.hin.mln.ibcn@dacim" class="oemail">vog.hin.mln.ibcn@dacim</a>
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</div></div></div><p class="small">Created: <span itemprop="datePublished">March 20, 2008</span>; Last Update: <span itemprop="dateModified">April 22, 2008</span>.</p></div><div class="jig-ncbiinpagenav body-content whole_rhythm" data-jigconfig="allHeadingLevels: ['h2'],smoothScroll: false" itemprop="text"><div id="LuLS172.T1" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK23169/table/LuLS172.T1/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__LuLS172.T1_lrgtbl__"><table><tbody><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Chemical name:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>177</sup>Lu-DOTA-Tyr<sup>3</sup>-c(Cys-Tyr-Trp-Lys-Thr-Cys)-Thr-Lys(cypate)-NH<sub>2</sub></td><td rowspan="9" colspan="1" style="text-align:left;vertical-align:middle;"></td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Abbreviated name:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>177</sup>Lu-LS172</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Synonym:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>177</sup>Lu-DOTA-Tyr<sup>3</sup>-octreotate-Lys-cypate, <sup>177</sup>Lu-DOTA-Y3-TATE-Lys-cypate</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Agent category:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Peptide</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Target:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Somatostatin receptor subtype-2 (SSTR-2)</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Target category:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Receptor</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Method of detection:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Single-photon emission computed tomography (SPECT), near-infrared (NIR) fluorescent imaging, optical fluorescent imaging</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Source of signal/contrast:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><sup>177</sup>Lu, cypate</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Activation:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">No</td></tr><tr><td rowspan="1" colspan="1" style="text-align:right;vertical-align:top;">
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<b>Studies:</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<ul class="simple-list"><li class="half_rhythm"><div>
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" />
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<i>In vitro</i>
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</div></li></ul>
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<ul class="simple-list"><li class="half_rhythm"><div>
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<img alt="Checkbox" src="/corehtml/pmc/css/bookshelf/2.26/img/studies.checkbox.png" /> Rodents
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</div></li></ul>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">No structure is currently available in <a href="http://pubchem.ncbi.nlm.nih.gov" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubChem</a>.</td></tr></tbody></table></div></div><div id="LuLS172.Background"><h2 id="_LuLS172_Background_">Background</h2><p>[<a href="/sites/entrez?Db=pubmed&Cmd=DetailsSearch&Term=177Lu%20+%20LS172" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>Somatostatin (SST) (somatotropin release-inhibiting hormone, somatotropin release-inhibiting factor) is a cyclic disulphide-containing peptide hormone of 14 amino acids (<a class="bk_pop" href="#LuLS172.REF.1">1</a>). SST inhibits hormone secretion, cell proliferation, and promotes apoptosis through binding to specific cell-surface somatostatin receptors (SSTRs) (<a class="bk_pop" href="#LuLS172.REF.2">2</a>). Five SSTR subtypes are identified in the central nervous system (CNS), gastrointestinal tract, and a variety of benign and malignant tumors (<a class="bk_pop" href="#LuLS172.REF.2">2</a>). All subtypes of SSTRs belong to the family of G protein–coupled receptors, and exhibit high affinity to SST by recognizing the β-turn in the peptide sequence of SST including Phe7, Trp8, Lys9, and Thr10 (<a class="bk_pop" href="#LuLS172.REF.2">2</a>). The structural difference between SSTRs generates specific pharmacological and physiological properties for each subtype, which allows targeting of SSTRs with subtype-specific SST analogs (<a class="bk_pop" href="#LuLS172.REF.1">1</a>). For example, octreotide, a SST analog with a peptide sequence of eight amino acids (D-Phe-c(Cys-Tyr-D-Trp-Lys-Thr-Cys)-Thr(ol)), possesses a much higher affinity (~2 nM) binding to SSTR-2, -3, and -5 than binding to SSTR-1 and -4 (>1,000 nM). In addition to symptomatic treatment of tumors in clinic, these analogs are also labeled with a variety of probes for imaging (<a class="bk_pop" href="#LuLS172.REF.1">1</a>).</p><p><sup>177</sup>Lu-DOTA-Tyr<sup>3</sup>-c(Cys-Tyr-Trp-Lys-Thr-Cys)-Thr-Lys(cypate)-NH<sub>2</sub>(<sup>177</sup>Lu-LS172) is a monomolecular multimodal imaging agent (MOMIA) for single-photon emission computed tomography (SPECT) and optical imaging (<a class="bk_pop" href="#LuLS172.REF.3">3</a>). <sup>177</sup>Lu-LS172 consists of three components: a STT analog Tyr3-octreotate (Y3-TATE) with an additional lysine at the N-terminal as a spacer linker, a complex of <sup>177</sup>Lu-1,4,7,10-tetraazacyclododecane-<i>N,N',N'',N'''</i>-tetraacetic acid (<sup>177</sup>Lu-DOTA) attached at the C-terminal of Y3-TATE, and a cypate attached at the ε-amine group of the spacer lysine at the N-terminal of Y3-TATE. As a STT analog, TATE is produced by replacing the C-terminal threoninol in the octreotide with threonine, which substantially increases the binding affinity for SSTR-2 (<a class="bk_pop" href="#LuLS172.REF.1">1</a>). <sup>177</sup>Lu is a radionuclide belonging to the group of rare earth isotopes, and it is produced by neutron bombardment of purified target materials in reactors (<a class="bk_pop" href="#LuLS172.REF.4">4</a>). With a half-life of 6.71 days for β<sup>-</sup> emission at 498 keV and 78% branch fraction, <sup>177</sup>Lu has been a very promising radionuclide in radiotherapy for effectively destroying small tumors and metastasis (optimal size 1.2–3.0 mm) while sparing normal tissue (<a class="bk_pop" href="#LuLS172.REF.5">5</a>). <sup>177</sup>Lu also emits low energetic gamma rays at 208 and 113 keV with 10% and 6% abundance, respectively, which allows for direct monitoring of the activity distribution by SPECT and subsequent dosimetry (<a class="bk_pop" href="#LuLS172.REF.5">5</a>). <sup>177</sup>Lu-DOTA-Y3-TATE has demonstrated excellent tumor localization, good clearance properties, and significant tumor regression in animal models (<a class="bk_pop" href="#LuLS172.REF.6">6</a>). Cypate (mw 625.34) is a carbocyanine derivative with structure and optical properties very similar to indocyanine green dye (ICG). Cypate exhibits a high extinction coefficient (224,000 M<sup>-1</sup>cm<sup>-1</sup>) in the near-infrared (NIR) region (700–900 nm) (<a class="bk_pop" href="#LuLS172.REF.3">3</a>, <a class="bk_pop" href="#LuLS172.REF.7">7</a>). The low light scattering and absorption of endogenous photoactive biomolecules in this region permit photons to penetrate several centimeters into tissues (<a class="bk_pop" href="#LuLS172.REF.8">8</a>, <a class="bk_pop" href="#LuLS172.REF.9">9</a>). Two carboxyl groups in cypate can be conjugated with amines to generate peptide-based optical imaging agents (<a class="bk_pop" href="#LuLS172.REF.10">10</a>).</p></div><div id="LuLS172.Synthesis"><h2 id="_LuLS172_Synthesis_">Synthesis</h2><p>[<a href="/sites/entrez?Db=pubmed&Cmd=DetailsSearch&Term=(177Lu%20+%20LS172)+AND+synthesis%0D%0A" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>The synthesis of <sup>177</sup>Lu-LS172 was conducted in several steps (<a class="bk_pop" href="#LuLS172.REF.3">3</a>). Y3-TATE was synthesized with a peptide synthesizer by standard automated Fmoc protocols. Rink amide resin was initially loaded with Fmoc amino acids followed by automatic activation of the carboxyl group with a mixture of 1-hydroxybenzotriazole (HOBt) and <i>o</i>-(benzotriazol-1-yl)-<i>N</i>,<i>N</i>,<i>N</i>',<i>N</i>'-tetramethyluronium hexafluorophosphate (HBTU) and subsequent coupling with Fmoc-protected amino acid. LS172 was produced by attaching DOTA and cypate to Y3-TATE <i>in situ</i>. The carboxylic acid of tri-t-butyl-DOTA was coupled to the amine of the N-terminal phenylalanine, and the carboxylic acid of cypate was coupled to the ε-amino group of the C-terminal lysine. The overall yield of LS172 was found to be 96%. The radiolabling of LS172 was accomplished by mixing <sup>177</sup>LuCl<sub>3</sub> (100 μCi) with LS172 in a buffer (pH 4.0) and incubated at 80ºC for 80 min. The produced <sup>177</sup>Lu-LS172 had a radiochemical purity of ≥99% and a final specific activity of 12.5 Ci/g (27 Ci/mmol).</p></div><div id="LuLS172.In_Vitro_Studies_Tes"><h2 id="_LuLS172_In_Vitro_Studies_Tes_"><i>In Vitro</i> Studies: Testing in Cells and Tissues</h2><p>[<a href="/sites/entrez?Db=pubmed&Cmd=DetailsSearch&Term=(177Lu%20+%20LS172)+AND+%22in+vitro%22" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>The spectral and binding properties of LS172 were examined <i>in vitro</i> (<a class="bk_pop" href="#LuLS172.REF.3">3</a>). Similar to cypate, LS172 exhibited broad excitation and emission bands with a narrow Stokes shift (23 nm). The relative quantum yield of LS172 (0.12) was the same as that of ICG. Because of the modifications in both C- and N-terminal, the affinity of LS172 binding to SSTR-2 increased ~10- and ~5-fold relative to cypate-Y3-TATE and Y3-TATE, respectively. The complexation with Lu<sup>3+</sup> appeared not to affect the resultant affinity (2.14 nM for Lu-LS172 <i>versus</i> 2.03 nM for LS172). The internalization of LS172 was evaluated with NIR fluorescence microscopy in A427-7 membranes (SSTR-2–positive) and HEK293 cells (STTR-2–negative). LS172 was weakly internalized at 25 nM. The internalization was inhibited by 5 μM Y3-TATE with an incubation time <60 min. In comparison, cypate-Y3-TATE was strongly internalized in a time-dependent manner, and the internalization was completely blocked by 5 μM Y3-TATE.</p></div><div id="LuLS172.Animal_Studies"><h2 id="_LuLS172_Animal_Studies_">Animal Studies</h2><div id="LuLS172.Rodents"><h3>Rodents</h3><p>[<a href="/sites/entrez?Db=pubmed&Cmd=DetailsSearch&Term=(177Lu%20+%20LS172)%20+AND++rodentia" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>The biochemical distribution of LS172 was examined in AR42J tumors in rats (<i>n</i> = 5) (<a class="bk_pop" href="#LuLS172.REF.3">3</a>). <sup>177</sup>Lu-LS172 (6.2 Ci/230 mmol (500 mg/230 mmol)) was injected intravenously in rats at 10–14 days after tumor implantation in the legs or after the tumors had grown ~1.5–2.0 g. In another group of tumor-implanted rats (<i>n</i> = 5), Y3-TATE (100μg/95 nmol) was also included as a competitive dose in addition to the radiolabeled LS172. The pharmacokinetic profile <sup>177</sup>Lu-LS172 exhibited a rapid blood clearance of 0.228 ± 0.047% injected dose per gram (ID/g) (0.151 ± 0.027% ID/g) at 1 h after injection. Clearance of <sup>177</sup>Lu-LS172 was predominately hepatic (17.862 ± 3.286% ID/g, 89.6 ± 3.16% ID/liver, 1 h) with relatively low kidney accumulation (1–2%). Accumulation of activity for <sup>177</sup>Lu-LS172 in the SSTR-2–positive tissues of adrenal, pituitary, pancreas, and tumor were relatively low (≤1% ID/g). With a co-administration of Y3-TATE, the accumulation of <sup>177</sup>Lu-LS172 decreased significantly in all SSTR-2–positive tissue except the bone.</p><p>The NIR fluorescence imaging of LS172 was performed in tumor-bearing NCR nu/nu mice (<i>n</i> = 6) (<a class="bk_pop" href="#LuLS172.REF.3">3</a>). After inoculation with lung adenocarcinoma cell line A427-7 in the right and left flanks of each mouse, tumors were allowed to grow to 5–10 mm maximum diameter before imaging. Three mice were injected with 2 nmol LS172, and two other mice were injected with 2 nmol LS172 and a competitive dose of 95 nmol Y3-TATE. NIR fluorescence images were collected at 1, 4, 8, and 24 h after injection. No significant accumulation of LS172 was found in tumors compared to that in normal tissue at different time points. The competitive inhibition with Y3-TATE did not significantly alter the tumor/muscle uptake ratio. After 24 h, the mice were euthanized, and tissues were harvested for <i>ex vivo</i> fluorescence biodistribution imaging. In addition to the liver and kidneys, LS172 accumulated in the spleen and accounted for 35% of the fluorescence intensity relative to that in the liver. LS172 accumulation in mouse kidney was somewhat higher than that of the radiolabeled analogs in rat kidneys, possibly indicating the reduction of overall charge on the DOTA upon chelation with a metal ion. The uptake and clearance profiles of LS172 in tumor-bearing A427-7 mice were similar to those of <sup>177</sup>Lu-LS172 in tumor-bearing AR427 rats.</p></div><div id="LuLS172.Other_NonPrimate_Mam"><h3>Other Non-Primate Mammals</h3><p>[<a href="/entrez/query.fcgi?cmd=PureSearch&db=pubmed&details_term=%22%20SUBSTANCENAME%22%5BSubstance%20Name%5D%20AND%20%28dog%20OR%20rabbit%20OR%20pig%20OR%20sheep%29" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div><div id="LuLS172.NonHuman_Primates"><h3>Non-Human Primates</h3><p>[<a href="/sites/entrez?Db=pubmed&Cmd=DetailsSearch&Term=(177Lu%20+%20LS172)%20+AND+(primate+non+human)" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p></div></div><div id="LuLS172.Human_Studies"><h2 id="_LuLS172_Human_Studies_">Human Studies</h2><p>[<a href="/sites/entrez?Db=pubmed&Cmd=DetailsSearch&Term=(177Lu%20+%20LS172)%20+AND+human" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">PubMed</a>]</p><p>No publication is currently available.</p><div id="LuLS172.NIH_Support"><h3>NIH Support</h3><p>CA 100972, EB 1430, CA 123537, CA 64475</p></div></div><div id="LuLS172.references"><h2 id="_LuLS172_references_">References</h2><dl class="temp-labeled-list"><dt>1.</dt><dd><div class="bk_ref" id="LuLS172.REF.1">Breeman W.A. , Kwekkeboom D.J. , de Blois E. , de Jong M. , Visser T.J. , Krenning E.P. Radiolabelled regulatory peptides for imaging and therapy. <span><span class="ref-journal">Anticancer Agents Med Chem. </span>2007;<span class="ref-vol">
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<strong>7</strong>
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</span>(3):345–57.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17504160" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17504160</span></a>]</div></dd><dt>2.</dt><dd><div class="bk_ref" id="LuLS172.REF.2">Barnett P. Somatostatin and somatostatin receptor physiology. <span><span class="ref-journal">Endocrine. </span>2003;<span class="ref-vol">
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<strong>20</strong>
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</span>(3):255–64.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/12721505" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 12721505</span></a>]</div></dd><dt>3.</dt><dd><div class="bk_ref" id="LuLS172.REF.3">Edwards W.B. , Xu B. , Akers W. , Cheney P.P. , Liang K. , Rogers B.E. , Anderson C.J. , Achilefu S. Agonist-antagonist dilemma in molecular imaging: evaluation of a monomolecular multimodal imaging agent for the somatostatin receptor. <span><span class="ref-journal">Bioconjug Chem. </span>2008;<span class="ref-vol">
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<strong>19</strong>
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</span>(1):192–200.</span> [<a href="/pmc/articles/PMC2539107/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC2539107</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/18020401" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 18020401</span></a>]</div></dd><dt>4.</dt><dd><div class="bk_ref" id="LuLS172.REF.4">Schotzig U. , Schrader H. , Schonfeld E. , Gunther E. , Klein R. Standardisation and decay data of 177Lu and 188Re. <span><span class="ref-journal">Appl Radiat Isot. </span>2001;<span class="ref-vol">
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<strong>55</strong>
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</span>(1):89–96.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/11339536" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 11339536</span></a>]</div></dd><dt>5.</dt><dd><div class="bk_ref" id="LuLS172.REF.5">Dvorakova Z. , Henkelmann R. , Lin X. , Turler A. , Gerstenberg H. Production of 177Lu at the new research reactor FRM-II: Irradiation yield of 176Lu(n,gamma)177Lu. <span><span class="ref-journal">Appl Radiat Isot. </span>2008;<span class="ref-vol">
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<strong>66</strong>
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</span>(2):147–51.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/17900914" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 17900914</span></a>]</div></dd><dt>6.</dt><dd><div class="bk_ref" id="LuLS172.REF.6">de Jong M. , Breeman W.A. , Bernard B.F. , Bakker W.H. , Schaar M. , van Gameren A. , Bugaj J.E. , Erion J. , Schmidt M. , Srinivasan A. , Krenning E.P. [177Lu-DOTA(0),Tyr3] octreotate for somatostatin receptor-targeted radionuclide therapy. <span><span class="ref-journal">Int J Cancer. </span>2001;<span class="ref-vol">
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<strong>92</strong>
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</span>(5):628–33.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/11340564" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 11340564</span></a>]</div></dd><dt>7.</dt><dd><div class="bk_ref" id="LuLS172.REF.7">Achilefu S. , Dorshow R.B. , Bugaj J.E. , Rajagopalan R. Novel receptor-targeted fluorescent contrast agents for in vivo tumor imaging. <span><span class="ref-journal">Invest Radiol. </span>2000;<span class="ref-vol">
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<strong>35</strong>
|
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</span>(8):479–85.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/10946975" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 10946975</span></a>]</div></dd><dt>8.</dt><dd><div class="bk_ref" id="LuLS172.REF.8">Mahmood U. , Weissleder R. Near-infrared optical imaging of proteases in cancer. <span><span class="ref-journal">Mol Cancer Ther. </span>2003;<span class="ref-vol">
|
||
<strong>2</strong>
|
||
</span>(5):489–96.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/12748311" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 12748311</span></a>]</div></dd><dt>9.</dt><dd><div class="bk_ref" id="LuLS172.REF.9">Ye Y. , Bloch S. , Xu B. , Achilefu S. Novel near-infrared fluorescent integrin-targeted DFO analogue. <span><span class="ref-journal">Bioconjug Chem. </span>2008;<span class="ref-vol">
|
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<strong>19</strong>
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</span>(1):225–34.</span> [<a href="/pmc/articles/PMC2631379/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC2631379</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/18038965" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 18038965</span></a>]</div></dd><dt>10.</dt><dd><div class="bk_ref" id="LuLS172.REF.10">Zhang Z. , Achilefu S. Spectral properties of pro-multimodal imaging agents derived from a NIR dye and a metal chelator. <span><span class="ref-journal">Photochem Photobiol. </span>2005;<span class="ref-vol">
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<strong>81</strong>
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</span>(6):1499–504.</span> [<a href="https://pubmed.ncbi.nlm.nih.gov/16120005" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 16120005</span></a>]</div></dd></dl></div><div id="bk_toc_contnr"></div></div></div>
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<div class="post-content"><div><div class="half_rhythm"><a href="/books/about/copyright/">Copyright Notice</a></div><div class="small"><span class="label">Bookshelf ID: NBK23169</span><span class="label">PMID: <a href="https://pubmed.ncbi.nlm.nih.gov/20641372" title="PubMed record of this page" ref="pagearea=meta&targetsite=entrez&targetcat=link&targettype=pubmed">20641372</a></span></div><div style="margin-top:2em" class="bk_noprnt"><a class="bk_cntns" href="/books/n/micad/">Contents</a><div class="pagination bk_noprnt"><a class="active page_link prev" href="/books/n/micad/sos177lucypate/" title="Previous page in this title">< Prev</a><a class="active page_link next" href="/books/n/micad/sos64cucy5.5/" title="Next page in this title">Next ></a></div></div></div></div>
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<div xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance"></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Views</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="PDF_download" id="Shutter"></a></div><div class="portlet_content"><ul xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="simple-list"><li><a href="/books/NBK23169/?report=reader">PubReader</a></li><li><a href="/books/NBK23169/?report=printable">Print View</a></li><li><a data-jig="ncbidialog" href="#_ncbi_dlg_citbx_NBK23169" data-jigconfig="width:400,modal:true">Cite this Page</a><div id="_ncbi_dlg_citbx_NBK23169" style="display:none" title="Cite this Page"><div class="bk_tt">Zhang H. 177Lu-DOTA-Tyr3-c(Cys-Tyr-Trp-Lys-Thr-Cys)-Thr-Lys(cypate)-NH2. 2008 Mar 20 [Updated 2008 Apr 22]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013. <span class="bk_cite_avail"></span></div></div></li><li><a href="/books/NBK23169/pdf/Bookshelf_NBK23169.pdf">PDF version of this page</a> (134K)</li><li><a href="/books/n/micad/toc/bin/micad.csv">MICAD summary (CSV file)</a></li></ul></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>In this page</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="page-toc" id="Shutter"></a></div><div class="portlet_content"><ul xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="simple-list"><li><a href="#LuLS172.Background" ref="log$=inpage&link_id=inpage">Background</a></li><li><a href="#LuLS172.Synthesis" ref="log$=inpage&link_id=inpage">Synthesis</a></li><li><a href="#LuLS172.In_Vitro_Studies_Tes" ref="log$=inpage&link_id=inpage"><i>In Vitro</i> Studies: Testing in Cells and Tissues</a></li><li><a href="#LuLS172.Animal_Studies" ref="log$=inpage&link_id=inpage">Animal Studies</a></li><li><a href="#LuLS172.Human_Studies" ref="log$=inpage&link_id=inpage">Human Studies</a></li><li><a href="#LuLS172.references" ref="log$=inpage&link_id=inpage">References</a></li></ul></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Search MICAD</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="source-application" id="Shutter"></a></div><div class="portlet_content"><form xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" name="frmSearch" method="get" action="/books/NBK5330/" id="frmSearch"><script type="text/javascript" src="/corehtml/pmc//js/bookshelf/micad.js">/**/</script><label class="offscreen_noflow" for="txtfield">Search term</label><input id="txtfield" type="text" name="f1_term" size="22" onKeyPress="KeyPress('micad',event,'/books/NBK5330/','')" /><button name="f1_search" type="submit">Go</button><button onclick="this.form.reset();" type="reset">Clear</button><p><b>Limit my Search:</b></p><div class="clearfix"><label for="detection">Method of detection:</label><div class="right"><select name="detection" id="detection" style="width:200px"><option value="" selected="selected">Any</option><option value="(MRI OR "Magnetic resonance imaging" OR MRS)">MRI</option><option value="Multimodal">Multimodal imaging</option><option value="Optical">Optical imaging</option><option value="PET">PET</option><option value="Photoacoustic">Photoacoustic imaging</option><option value="(SPECT OR planar)">SPECT</option><option value="Ultrasound">Ultrasound</option><option value="(x-ray OR ct)">X-ray, CT</option></select></div></div><div class="clearfix"><label for="signal">Source of signal/contrast:</label><div class="right"><select name="signal" id="signal" style="width:200px"><option value="" selected="selected">Any</option><optgroup label="MRI agents"><option value="(Copper OR Cu)">Copper</option><option value="(Europium OR Eu3+)">Europium</option><option value="(Fluorine OR 19F)">Fluorine</option><option value="(Gadolinium OR Gd3+)">Gadolinium</option><option value=""Hyperpolarized 13C"">Hyperpolarized 13C</option><option value=""Iron oxide"">Iron oxide</option><option value=""Nitroxide radicals"">Nitroxide radicals</option><option value="(Oxygen OR 17O)">Oxygen</option><option value="Thulium">Thulium</option></optgroup><optgroup label="Multimodal agents"><option value="((Gadolinium OR Gd3+) AND Optical)">Gadolinium and optical</option><option value="((Gadolinium OR Gd3+) AND (Gold OR Au))">Gadolinium and Gold</option><option value="("Iron oxide" AND (64Cu OR 124I OR 111In))">Iron oxide and
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value="("Nitrogen 13" OR 13N)">Nitrogen-13</option><option value="("Yttrium 86" OR 86Y)">Yttrium-86</option><option value="("Zirconium 89" OR 89Zr)">Zirconium-89</option></optgroup><optgroup label="Photoacoustic agents"><option value="(Gold OR Au)">Gold</option><option value="("Indocyanine green" OR ICG)">Indocyanine green</option></optgroup><optgroup label="SPECT radionuclides"><option value="(Gallium-67 OR 67Ga)">Gallium-67</option><option value="("Indium 111" OR 111In)">Indium-111</option><option value="("Iodine 123" OR "Iodine 125" OR "Iodine 131" OR 123I OR 125I OR 131I)">Iodine-123, 125, 131</option><option value="("Lutetium 177" OR 177Lu)">Lutetium-177</option><option value="(Rhenium OR 186Re OR 188Re)">Rhenium</option><option value="("Technetium 99m" OR 99mTc)">Technetium-99m</option><option value="("Tellurium 125m" OR 125mTe)">Tellurium-125m</option></optgroup><optgroup label="Ultrasound agents"><option value="Microbubbles">Microbubbles</option><option 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href="/books/?Db=pubmed&DbFrom=books&Cmd=Link&LinkName=books_pubmed_refs&IdsFromResult=1504158" ref="log$=recordlinks">PubMed</a><div class="brieflinkpop offscreen_noflow">Links to PubMed</div></li></ul></div></div><div class="portlet"><div class="portlet_head"><div class="portlet_title"><h3><span>Similar articles in PubMed</span></h3></div><a name="Shutter" sid="1" href="#" class="portlet_shutter" title="Show/hide content" remembercollapsed="true" pgsec_name="PBooksDiscovery_RA" id="Shutter"></a></div><div class="portlet_content"><ul><li class="brieflinkpopper two_line"><a class="brieflinkpopperctrl" href="/pubmed/20641431" ref="ordinalpos=1&linkpos=1&log$=relatedreviews&logdbfrom=pubmed"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> (64)Cu-DOTA-Tyr(3)-c(Cys-Tyr-Trp-Lys-Thr-Cys)-Thr-Lys(cypate)-NH(2).</a><span class="source">[Molecular Imaging and Contrast...]</span><div class="brieflinkpop offscreen_noflow"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> (64)Cu-DOTA-Tyr(3)-c(Cys-Tyr-Trp-Lys-Thr-Cys)-Thr-Lys(cypate)-NH(2).<div class="brieflinkpopdesc"><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="author">Zhang H. </em><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="cit">Molecular Imaging and Contrast Agent Database (MICAD). 2004</em></div></div></li><li class="brieflinkpopper two_line"><a class="brieflinkpopperctrl" href="/pubmed/21290631" ref="ordinalpos=1&linkpos=2&log$=relatedreviews&logdbfrom=pubmed"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> (177)Lu-Labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-d-Trp-Lys-Thr-Cys)).</a><span class="source">[Molecular Imaging and Contrast...]</span><div class="brieflinkpop offscreen_noflow"><span xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="invert">Review</span> (177)Lu-Labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-Tyr-cyclo(DAB-Arg-cyclo(Cys-Phe-d-Trp-Lys-Thr-Cys)).<div class="brieflinkpopdesc"><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="author">Shan L. </em><em xmlns:np="http://ncbi.gov/portal/XSLT/namespace" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" class="cit">Molecular Imaging and Contrast Agent Database (MICAD). 2004</em></div></div></li><li class="brieflinkpopper two_line"><a class="brieflinkpopperctrl" href="/pubmed/20641308" ref="ordinalpos=1&linkpos=3&log$=relatedreviews&logdbfrom=pubmed"><span 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